Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048
Identifieur interne : 000E25 ( Main/Exploration ); précédent : 000E24; suivant : 000E26Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048
Auteurs : Molahlehi S. Sonopo [Afrique du Sud] ; Adushan Pillay [Afrique du Sud] ; Kelly Chibale [Afrique du Sud] ; Biljana Marjanovic-Painter [Afrique du Sud] ; Cristina Donini [Suisse] ; Jan R. Zeevaart [Afrique du Sud]Source :
- Journal of Labelled Compounds and Radiopharmaceuticals [ 0362-4803 ] ; 2016-12.
Abstract
The antimalarial compound MMV390048 ([14C]‐11) was labeled with carbon‐14 isotope via a 3‐step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon‐14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [14C]‐11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues. The radioactivity uptake was higher in the eyes of the pigmented rats than in the eyes of the albino rats at all‐time points. The highest accumulation reached in the eyes of the pigmented rats was 0.46% at 6 hours. However, these levels are still very low as compared to the other organs studied. There was very little radioactivity from MMV390048 ([14C]‐11) present in the skin of both the albino and pigmented rats. The results obtained are supportive of further development of MMV390048 as a potential antimalarial compound.
The antimalarial compound MMV390048 ([14C]‐11) was labeled with carbon‐14 isotope via a 3‐step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon‐14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [14C]‐11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues.
Url:
DOI: 10.1002/jlcr.3445
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Istex, to step Corpus: 000888
- to stream Istex, to step Curation: 000888
- to stream Istex, to step Checkpoint: 000044
- to stream Main, to step Merge: 000E26
- to stream Main, to step Curation: 000E25
Le document en format XML
<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title xml:lang="en">Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048</title><author><name sortKey="Sonopo, Molahlehi S" sort="Sonopo, Molahlehi S" uniqKey="Sonopo M" first="Molahlehi S." last="Sonopo">Molahlehi S. Sonopo</name></author><author><name sortKey="Pillay, Adushan" sort="Pillay, Adushan" uniqKey="Pillay A" first="Adushan" last="Pillay">Adushan Pillay</name></author><author><name sortKey="Chibale, Kelly" sort="Chibale, Kelly" uniqKey="Chibale K" first="Kelly" last="Chibale">Kelly Chibale</name></author><author><name sortKey="Marjanovic Ainter, Biljana" sort="Marjanovic Ainter, Biljana" uniqKey="Marjanovic Ainter B" first="Biljana" last="Marjanovic-Painter">Biljana Marjanovic-Painter</name></author><author><name sortKey="Donini, Cristina" sort="Donini, Cristina" uniqKey="Donini C" first="Cristina" last="Donini">Cristina Donini</name></author><author><name sortKey="Zeevaart, Jan R" sort="Zeevaart, Jan R" uniqKey="Zeevaart J" first="Jan R." last="Zeevaart">Jan R. Zeevaart</name></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:10457EC7AB181B1F5CBA50CB73EA728698C8F8D8</idno><date when="2016" year="2016">2016</date><idno type="doi">10.1002/jlcr.3445</idno><idno type="url">https://api.istex.fr/ark:/67375/WNG-759SLKTJ-Z/fulltext.pdf</idno><idno type="wicri:Area/Istex/Corpus">000888</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">000888</idno><idno type="wicri:Area/Istex/Curation">000888</idno><idno type="wicri:Area/Istex/Checkpoint">000044</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">000044</idno><idno type="wicri:doubleKey">0362-4803:2016:Sonopo M:carbon:radiolabeling:and</idno><idno type="wicri:Area/Main/Merge">000E26</idno><idno type="wicri:Area/Main/Curation">000E25</idno><idno type="wicri:Area/Main/Exploration">000E25</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a" type="main">Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048</title><author><name sortKey="Sonopo, Molahlehi S" sort="Sonopo, Molahlehi S" uniqKey="Sonopo M" first="Molahlehi S." last="Sonopo">Molahlehi S. Sonopo</name><affiliation wicri:level="1"><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>Radiochemistry, Necsa, Pretoria</wicri:regionArea><wicri:noRegion>Pretoria</wicri:noRegion></affiliation><affiliation wicri:level="1"><country wicri:rule="url">Afrique du Sud</country></affiliation><affiliation></affiliation><affiliation wicri:level="1"><country wicri:rule="url">Afrique du Sud</country></affiliation></author><author><name sortKey="Pillay, Adushan" sort="Pillay, Adushan" uniqKey="Pillay A" first="Adushan" last="Pillay">Adushan Pillay</name><affiliation wicri:level="1"><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>Radiochemistry, Necsa, Pretoria</wicri:regionArea><wicri:noRegion>Pretoria</wicri:noRegion></affiliation></author><author><name sortKey="Chibale, Kelly" sort="Chibale, Kelly" uniqKey="Chibale K" first="Kelly" last="Chibale">Kelly Chibale</name><affiliation wicri:level="1"><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>Drug Discovery and Development Centre (H3D) and South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry, University of Cape Town, Rondebosch</wicri:regionArea><wicri:noRegion>Rondebosch</wicri:noRegion></affiliation></author><author><name sortKey="Marjanovic Ainter, Biljana" sort="Marjanovic Ainter, Biljana" uniqKey="Marjanovic Ainter B" first="Biljana" last="Marjanovic-Painter">Biljana Marjanovic-Painter</name><affiliation wicri:level="1"><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>Radiochemistry, Necsa, Pretoria</wicri:regionArea><wicri:noRegion>Pretoria</wicri:noRegion></affiliation></author><author><name sortKey="Donini, Cristina" sort="Donini, Cristina" uniqKey="Donini C" first="Cristina" last="Donini">Cristina Donini</name><affiliation wicri:level="1"><country xml:lang="fr">Suisse</country><wicri:regionArea>Translational Medicine, MMV, Geneva</wicri:regionArea><wicri:noRegion>Geneva</wicri:noRegion></affiliation></author><author><name sortKey="Zeevaart, Jan R" sort="Zeevaart, Jan R" uniqKey="Zeevaart J" first="Jan R." last="Zeevaart">Jan R. Zeevaart</name><affiliation wicri:level="1"><country xml:lang="fr">Afrique du Sud</country><wicri:regionArea>DST/NWU, Preclinical Drug Development Platform, North‐West University, Potchefstroom</wicri:regionArea><wicri:noRegion>Potchefstroom</wicri:noRegion></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Labelled Compounds and Radiopharmaceuticals</title><title level="j" type="sub">IIS 2015 Princeton Conference</title><title level="j" type="alt">JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS</title><idno type="ISSN">0362-4803</idno><idno type="eISSN">1099-1344</idno><imprint><biblScope unit="vol">59</biblScope><biblScope unit="issue">14</biblScope><biblScope unit="page" from="680">680</biblScope><biblScope unit="page" to="688">688</biblScope><biblScope unit="page-count">9</biblScope><date type="published" when="2016-12">2016-12</date></imprint><idno type="ISSN">0362-4803</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0362-4803</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract">The antimalarial compound MMV390048 ([14C]‐11) was labeled with carbon‐14 isotope via a 3‐step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon‐14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [14C]‐11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues. The radioactivity uptake was higher in the eyes of the pigmented rats than in the eyes of the albino rats at all‐time points. The highest accumulation reached in the eyes of the pigmented rats was 0.46% at 6 hours. However, these levels are still very low as compared to the other organs studied. There was very little radioactivity from MMV390048 ([14C]‐11) present in the skin of both the albino and pigmented rats. The results obtained are supportive of further development of MMV390048 as a potential antimalarial compound.</div><div type="abstract">The antimalarial compound MMV390048 ([14C]‐11) was labeled with carbon‐14 isotope via a 3‐step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon‐14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [14C]‐11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues.</div></front></TEI><affiliations><list><country><li>Afrique du Sud</li><li>Suisse</li></country></list><tree><country name="Afrique du Sud"><noRegion><name sortKey="Sonopo, Molahlehi S" sort="Sonopo, Molahlehi S" uniqKey="Sonopo M" first="Molahlehi S." last="Sonopo">Molahlehi S. Sonopo</name></noRegion><name sortKey="Chibale, Kelly" sort="Chibale, Kelly" uniqKey="Chibale K" first="Kelly" last="Chibale">Kelly Chibale</name><name sortKey="Marjanovic Ainter, Biljana" sort="Marjanovic Ainter, Biljana" uniqKey="Marjanovic Ainter B" first="Biljana" last="Marjanovic-Painter">Biljana Marjanovic-Painter</name><name sortKey="Pillay, Adushan" sort="Pillay, Adushan" uniqKey="Pillay A" first="Adushan" last="Pillay">Adushan Pillay</name><name sortKey="Sonopo, Molahlehi S" sort="Sonopo, Molahlehi S" uniqKey="Sonopo M" first="Molahlehi S." last="Sonopo">Molahlehi S. Sonopo</name><name sortKey="Sonopo, Molahlehi S" sort="Sonopo, Molahlehi S" uniqKey="Sonopo M" first="Molahlehi S." last="Sonopo">Molahlehi S. Sonopo</name><name sortKey="Zeevaart, Jan R" sort="Zeevaart, Jan R" uniqKey="Zeevaart J" first="Jan R." last="Zeevaart">Jan R. Zeevaart</name></country><country name="Suisse"><noRegion><name sortKey="Donini, Cristina" sort="Donini, Cristina" uniqKey="Donini C" first="Cristina" last="Donini">Cristina Donini</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000E25 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 000E25 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= ChloroquineV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= ISTEX:10457EC7AB181B1F5CBA50CB73EA728698C8F8D8
|texte= Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048
}}
| This area was generated with Dilib version V0.6.33. |  |